Triptolide lactone ring derivatives as immunomodulators and anticancer agents

Abstract

Disclosed are compounds based on lactone ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.

It is claimed: 
     
       1. A compound having the structure II: 
       
         
           
           
               
               
           
         
       
       where
 each R 6  is independently selected from alkyl, alkenyl, alkynyl, or aryl; 
 CR 2 R 3  is CHOH or C═O; 
 at most one of the groups X is hydroxyl, and the remaining groups X are hydrogen. 
 
     
     
       2. The compound of  claim 1 , wherein CR 2 R 3  is CHOH. 
     
     
       3. The compound of  claim 2 , wherein CR 2 R 3  is CHOH (β-hydroxy). 
     
     
       4. The compound of  claim 1 , wherein each X is hydrogen. 
     
     
       5. The compound of  claim 1 , wherein each said alkyl, alkenyl, and alkynyl includes at most four carbon atoms, and each said aryl is monocyclic and non-heterocyclic. 
     
     
       6. The compound of  claim 1 , wherein each R 6  is aryl. 
     
     
       7. The compound of  claim 6 , wherein each R 6  is phenyl.